Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis
Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis
复制标题
鉴定 Blapsins A 和 B 作为来自昆虫 Blaps japanensis 的有效小分子 14-3-3 抑制剂
DOI：
10.1016/j.bmcl.2012.04.027
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发表时间：
2012-06-15
影响因子：
2.7
通讯作者：
Cheng, Yong-Xian
中科院分区：
文献类型：
--
作者：
Yan, Yong-Ming;Dai, Huan-Qin;Cheng, Yong-Xian
在这项研究中，我们报告了三个新的天然存在的化合物，blapsins A（1）和B（2），和blapsamide（3）的乙醇提取物的臭甲虫，Blaps japanensis。利用光谱方法确定了这些化合物的结构。化合物3是在结构中带有甲酰胺基的酚类化合物。功能研究表明，化合物1和2有效地抑制14-3-3蛋白质-蛋白质相互作用（PPI），其IC 50值分别为9.2和10.0 μ M（通过ELISA测定）和2.0和2.5 μ M（在FP测定中）。这些化合物代表了天然小分子14-3-3抑制剂的第一个例子。(C)2012爱思唯尔有限公司保留所有权利。
In this study, we report three novel naturally occurring compounds, blapsins A (1) and B (2), and blapsamide (3) from the ethanol extract of the stink beetle, Blaps japanensis. The structures of these compounds were determined using spectroscopic methods. Compound 3 is a phenolic compound bearing a formamido group in the structure. Functional studies revealed that compounds 1 and 2 potently inhibited 14-3-3 protein-protein interactions (PPIs) with IC50 values of 9.2 and 10.0 mu M as determined by an ELISA assay, and 2.0 and 2.5 mu M in an FP assay, respectively. These compounds represent the first example of natural small-molecule 14-3-3 inhibitors. (C) 2012 Elsevier Ltd. All rights reserved.